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Current Molecular Pharmacology

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https://www.readbyqxmd.com/read/29921214/sepsis-the-involvement-of-platelets-and-the-current-treatments
#1
Ana Carolina Antunes Naime, Jessica Oliveira Frade Ganaes, Maria Elisa Lopes-Pires
OBJECTIVE: Sepsis, a serious and life threatening complication arising from infection caused by lipopolysaccharide, is a complex inflammatory syndrome, and one of the main causes of death in intensive care units (ICU). It is characterized as an over-response of pro-coagulant agents promotes coagulopathy and thrombus formation, resulting in disseminated intravascular coagulation (DIC). Furthermore, it can cause multiple organ dysfunction and hypotension (septic shock) resulting in death...
June 19, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29921213/radiation-protection-and-mitigation-by-natural-antioxidants-and-flavonoids-implications-to-radiotherapy-and-radiation-disasters
#2
Rasoul Yahyapour, Dheyauldeen Shabeeb, Mohsen Cheki, Ahmed Eleojo Musa, Bagher Farhood, Abolhasan Rezaeyan, Peyman Amini, Hengameh Fallah, Masoud Najafi
BACKGROUND: Nowadays, ionizing radiations are used for various medical and terroristic aims. These purposes involve exposure to ionizing radiations. Hence, people are at risk for acute or late effects. Annually, millions of cancer patients undergo radiotherapy during their course of treatment. Also, some radiological or nuclear events in recent years pose a threat to people, hence the need for radiation mitigation strategies. Amifostine, the first FDA approved radioprotector, has shown some toxicities that limit its usage and efficiency...
June 19, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29766831/phagocytosis-and-motility-in-human-neutrophils-is-competent-but-compromised-by-pharmacological-inhibition-of-ezrin-phosphorylation
#3
Rhiannon E Roberts, Geetha L Elumalai, Maurice B Hallett
BACKGROUND AND OBJECTIVE: Ezrin links the cortical cytoskeleton to the plasma membrane and plays a role in regulating cell shape change. Recently NSC668394 has been shown to inhibit a key step for its activity, i.e. phosphorylation at threonine 567. In neutrophils, another key regulatory step is the Ca2+-mediated cleavage of ezrin by calpain. METHODS: In this paper we use NSC668394 as a pharmacological inhibitor to investigate the interplay between these two steps in regulating neutrophil shape change...
May 15, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29766830/impact-of-sphingolipid-mediators-on-determination-of-cochlear-survival-in-ototoxicity
#4
Keiji Tabuchi, Akira Hara
BACKGROUND AND OBJECTIVE: Sphingolipid metabolites, including ceramide, sphingosine, and their phosphorylates (ceramide-1-phosphonate [C1P] and sphingosine-1-phosphate [S1P]), regulate diverse cellular processes including apoptosis, the cell cycle, and cellular differentiation. Recent studies have shown that these sphingolipid metabolites are generated in response to ototoxic agents and play important roles in determining the fate of cochlear hair cells in ototoxic injury. METHODS: This review summarizes the current knowledge on the roles of sphingolipid mediators in cochlear ototoxicity...
May 15, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29741145/tandem-mass-spectrometric-cell-wall-proteome-profiling-of-a-candida-albicans-hwp2-mutant-strain
#5
Andy Awad, Pamela El Khoury, Brigitte Wex, Roy A Khalaf
BACKGROUND: Candida albicans is present as part of the normal gut flora and detected in the oral cavities and GI tracts of around fifty percent of adults. Benign colonization can turn pathogenic causing a variety of mild to severe infections. In a pathogen, the cell wall and cell surface proteins are major antigenic determinants and drug targets as they are the primary structures that contact the host. Cell surface proteins perform a variety of functions necessary for virulence such as adhesion, host degradation, resistance to oxidative stress, and drug resistance...
May 9, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29676239/transdermal-delivery-of-at1-receptor-antagonists-reduce-blood-pressure-and-reveals-a-vasodilatory-effect-in-kidney-blood-vessels
#6
Michaila Michalatou, Maria Eleni Androutsou, Markos Antonopoulos, Demetrios V Vlahakos, George Agelis, Anthony Zulli, Tawar Qaradakhi, Kathleen Mikkelsen, Vasso Apostolopoulos, John Matsoukas
BACKGROUND: The Renin Angiotensin System (RAS) is pharmacologically targeted to reduce blood pressure, and patient compliance to oral medications is a clinical issue. The mechanisms of action of angiotensin receptor blockers (ARBs) in reducing blood pressure are not well understood, and is purported to be via a reduction of angiotensin II signaling. OBJECTIVE: We aimed to develop a transdermal delivery method for ARBs (losartan potassium and valsartan) and to determine if ARBs reveal a vasodilatory effect of the novel RAS peptide, alamandine...
April 19, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29485015/protein-tyrosine-phosphatase-as-potential-therapeutic-target-in-various-disorders
#7
Shivani Verma, Saurabh Sharma
Protein tyrosine phosphatase (PTP) class of enzymes functions in a unit with protein tyrosine kinases to regulate signaling pathways. Several members of the PTP family link to human disease predisposition such as PTP1B, SH2, DEP1, and inhibition of these enzymes may represent an effective palliative therapy. Protein tyrosine phosphatase inhibition has been intensively investigated as an important therapeutic target against metabolic syndrome and has been documented to improve hepatic insulin sensitivity, reduce liver triglycerides, cholesterol levels, and protects against endoplasmic reticulum (ER) stress...
February 26, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29468988/cox-2-in-radiotherapy-a-potential-target-for-radioprotection-and-radiosensitization
#8
Mohsen Cheki, Rasoul Yahyapour, Bagher Farhood, Abolhassan Rezaeyan, Dheyauldeen Shabeeb, Peyman Amini, Saeed Rezapoor, Masoud Najafi
BACKGROUND: Each year, millions of people die from cancer. Radiotherapy is one of the main treatment strategies for cancer patients. Despite the beneficial roles of treatment with radiation, several side effects may threaten normal tissues of patients in the years after treatment. Moreover, high incidences of second primary cancers may reduce therapeutic ratio of radiotherapy. The search for appropriate targets of radiosensitization of tumor cells as well as radioprotection of normal tissues is one of the most interesting aims in radiobiology...
February 18, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29376497/l-sulforaphane-confers-protection-against-oxidative-stress-in-an-in-vitro-model-of-age-related-macular-degeneration
#9
Nabeela Khadija Dulull, Daniel Anthony Dias, Thilini Rasika Thrimawithana, Faith Ai Ai Kwa
BACKGROUND: In age-related macular degeneration, oxidative damage and abnormal neovascularization in the retina are caused by the upregulation of vascular endothelium growth factor and reduced expression of Glutathione-S-transferase genes. Current treatments are only palliative. Compounds from cruciferous vegetables (e.g. L-Sulforaphane) have been found to restore normal gene expression levels in diseases including cancer via the activity of histone deacetylases and DNA methyltransferases, thus retarding disease progression...
January 25, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29357811/targeting-m3-muscarinic-receptors-for-colon-cancer-therapy
#10
Jessica Felton, Shien Hu, Jean-Pierre Raufman
BACKGROUND: Expression and activation of subtype-3 muscarinic receptors (M3R) plays an important role in the progression of colorectal neoplasia. METHODS: Herein, we describe the role of muscarinic receptors in colon cancer, focusing specifically on M3R, illustrate how M3R over-expression and activation of post-receptor signaling pathways potentiates tumor progression, and explore the efficacy and safety of a variety of therapeutic approaches that can target the molecules involved...
January 18, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29370747/editorial-corticotropin-releasing-factor-crf-and-its-receptors-from-structure-to-function-in-health-and-disease-part-ii
#11
EDITORIAL
George Liapakis
No abstract text is available yet for this article.
2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29370746/preface
#12
Michael Kahn
No abstract text is available yet for this article.
2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29034844/micrornas-cancer-and-diet-facts-and-new-exciting-perspectives
#13
Maria L Motti, Stefania D Angelo, Rosaria Meccariello
BACKGROUND: MicroRNAs (miRNAs) are small non-coding RNAs able to regulate gene expression at multiple levels. They are detected in tissues, blood, and other body fluids with high stability and have a recognized role in maintaining of tissue homeostasis. Aberrant expression profile of miRNAs has been observed in several diseases, primarily cancer. As a consequence, the analysis of miRNA signature has recognized diagnostic and prognostic role in human diseases, and the development of miRNA-based therapies is currently under investigation...
2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/28969582/gamma-decanolactone-improves-biochemical-parameters-associated-with-pilocarpine-induced-seizures-in-male-mice
#14
Pricila Pfluger, Gabriela Gregory Regner, Vanessa Rodrigues Coelho, Lucas Lima da Silva, Leopoldo Nascimento, Cassiana Macagnan Viau, Regis Adriel Zanette, Cleonice Hoffmann, Jaqueline Nascimento Picada, Jenifer Saffi, Patricia Pereira
BACKGROUND AND OBJECTIVE: Gamma-decanolactone (GD) is a monoterpene effective against seizures induced by pentylenetetrazole. The mechanism of action of GD is likely to be via glutamate antagonism. GD also inhibits intracellular reactive oxygen species (ROS) generation and the lipopolysaccharide-induced expression of inducible nitric oxide synthase (iNOS) and tumor necrosis factor-alpha (TNF-α) in vitro. Considering the neuropharmacological profile of GD studied so far, we investigated the effect of intraperitoneal administration of GD 100 and 300 mg/kg on pilocarpine (PIL)-induced status epilepticus (SE) in mice...
2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/28933312/characterization-of-imatinib-resistant-cml-leukemic-stem-initiating-cells-and-their-sensitivity-to-cbp-catenin-antagonists
#15
Yi Zhao, Kaijin Wu, Yongfeng Wu, Elizabeth Melendez, Goar Smbatyan, David Massiello, Michael Kahn
BACKGROUND AND OBJECTIVE: The development of the tyrosine kinase inhibitor Imatinib (IM) represents a milestone in CML (Chronic Myeloid Leukemia) treatment. However, it is not curative and patients develop IM resistance. IM resistance has been previously correlated with the emergence of drug-resistant LIC/LSC (Leukemia Initiating Cell/Leukemia Stem Cell) and increased nuclear catenin levels and enhanced Wnt signaling. It has been demonstrated previously that drug resistant CML LIC/LSC can be safely eliminated both in vitro and in vivo via disruption of the CBP/catenin interaction, utilizing the highly biochemically selective small molecule CBP/catenin antagonist ICG- 001...
2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/28933311/mg17-a-novel-triazole-derivative-abrogated-neuroinflammation-and-related-neurodegenerative-symptoms-in-rodents
#16
Gangadhar Matharasala, Ganesh Samala, Yogeeswari Perumal
BACKGROUND AND OBJECTIVE: The objective of present study is to explore multiple effects of the compound MG17 and relate them to achieve better therapeutic potential against neuroinflammation related disorders. We examined whether our compound is acting through regulating neuroinflammatory mediators. METHODS: We have done some preliminary behavioral studies to shortlist the derivatives using rodent models of peripheral nerve injury in our earlier publication and now we extended our screening studies to explore the test compounds efficacy on other related peripheral neurological disorders such as Streptozotocin- induced diabetic peripheral neuropathy (DPN) and methyl mercury (MeHg) induced neurodegeneration in rats...
2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/28762308/the-nephroprotective-effect-of-n-acetyl-l-cysteine-and-atorvastatin-against-imipenem-induced-nephrotoxicity
#17
Abeer M Rababa’h, Tamara B Hijjawi, Karem H Alzoubi, Saddam Al Demour, Mera A Ababneh
BACKGROUND AND OBJECTIVE: Imipenem has played an important role in the treatment of broad-spectrum bacterial infection. However, nephrotoxicity due to imipenem remains an important clinical challenge. The aim of this study is to test the hypothesis stating that N-acetyl-L-cysteine (NAC) and atorvastatin possess a nephroprotective effect against imipenem-induced nephrotoxicity. METHODS: Adult Sprague Dawley rats were randomly assigned into six groups (n=8-10 rats/group; total n=55)...
2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/28676005/opioids-in-the-frame-of-new-psychoactive-substances-network-a-complex-pharmacological-and-toxicological-issue
#18
Ludovic Ventura, Felix Carvalho, Ricardo Jorge Dinis-Oliveira
BACKGROUND: New psychoactive substances (NPS), often referred to as "legal highs" or "designer drugs", are derivatives and analogues of existing psychoactive drugs that are introduced in the recreational market to circumvent existing legislation on drugs of abuse. OBJECTIVE: This systematic review aims to gather the state of the art regarding chemical, molecular pharmacology and toxicological information of opioid class of NPS. METHODS: Chemical, pharmacological, toxicological and clinical effects of opioid class of NPS were searched in books and in PubMed (U...
2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/28382868/prooxidant-antioxidant-balance-and-antioxidant-properties-of-thuja-orientalis-l-a-potential-therapeutic-approach-for-diabetes-mellitus
#19
Daryoush H Alamdari, Malihe Aghasizadeh-Sharbaf, Maryam Mohadjerani, Gordon A Ferns, Amir Avan
BACKGROUND: Diabetes mellitus (DM) is a major health problem with an increasing global prevalence. It is usually associated with an imbalance between pro-oxidant mechanisms and antioxidant defenses, contributing to oxidative-stress, and this leads to an increased susceptibility to endothelial dysfunction, atherosclerosis, insulin-resistance and impaired-pancreatic β-cell function. OBJECTIVE: We have assessed the Prooxidant-antioxidant balance (PAB) and anti-hemolytic effect of Thuja orientalis L using the PAB assay and the analysis of hematological markers...
2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/28260504/the-crf-family-of-neuropeptides-and-their-receptors-mediators-of-the-central-stress-response
#20
Nina Dedic, Alon Chen, Jan M Deussing
BACKGROUND: Dysregulated stress neurocircuits, caused by genetic and/or environmental changes, underlie the development of many neuropsychiatric disorders. Corticotropin-releasing factor (CRF) is the major physiological activator of the hypothalamic-pituitary-adrenal (HPA) axis and consequently a primary regulator of the mammalian stress response. Together with its three family members, urocortins (UCNs) 1, 2, and 3, CRF integrates the neuroendocrine, autonomic, metabolic and behavioral responses to stress by activating its cognate receptors CRFR1 and CRFR2...
2018: Current Molecular Pharmacology
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